synthesis and anticonvulsant activity evaluation of 3-alkoxy-4-(4- (hexyloxy/heptyloxy)phenyl)-4h-1,2,4 -triazole
نویسندگان
چکیده
a series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4h-1,2,4-triazole was synthesized. the anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (mes) test and rotarod tests with intraperitoneally injected mice. among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4h-1,2,4-triazole (5f) was the most active one and also had the lowest toxicity. in the anti-mes potency test, it showed median effective dose (ed50) of 37.3mg/kg, median toxicity dose (td50) of 422.5 mg/kg, and the protective index (pi) of 11.3 which is much greater than the reference drug carbamazepine with pi value of 6.4. as well as demonstrating the anti-mes efficacy of compound 5f, its potency against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline were also established, with the results suggesting that gaba-mediated mechanisms might be involved in its anticonvulsant activity, such as enhancing of gabaergic neurotransmission or activity, activate gad or inhibit gaba-t, and gabaa-mediated mechanisms.
منابع مشابه
Synthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4- (hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole
A series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4H-1,2,4-triazole was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4H-1,2,4-triazole (5f) was the most active one and also had...
متن کاملSynthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4- (hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole
A series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4H-1,2,4-triazole was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4H-1,2,4-triazole (5f) was the most active one and also had...
متن کاملSynthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4-(hexyloxy/heptyloxy)phenyl)-4H-1,2,4 -triazole
A series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4H-1,2,4-triazole was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4H-1,2,4-triazole (5f) was the most active one and also had...
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The green synthesis of 5-(4-aminophenyl)-4-aryl-4H-1,2,4-triazole-3-thiol was achieved in four steps, In first step, 4-amino benzoic acid refluxed in ethanol along with catalyst Conc. Sulphuric acid to produce ethyl-4-amino benzoate I. Further compound I refluxed with hydrazine hydrate in ethanol to produce 4-amino benzohydrazide II. Compound II refluxed in ethanolic potassium hydroxide with ca...
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Two novel 3-amino-5-(4-choloro-2-phenoxyphenyl)-4H-1,2,4-triazole derivatives were prepared and their anticonvulsant activity was measured by evaluation of the ability of these compounds to protect mice against convulsion induced by lethal doses of pentylenetetrazole (PTZ). Diazepam (Sigma) was considered as a positive control drug with anticonvulsant effect [ED50 = 1.2 (0.5-1.9) mg/Kg]. Amongs...
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عنوان ژورنال:
iranian journal of pharmaceutical researchجلد ۱۴، شماره ۱، صفحات ۷۷-۸۷
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